Additional file 1: of In vitro and in vivo characterization of the JAK1 selectivity of upadacitinib (ABT-494)

Table S1. Upadacitinib Kinome Selectivity. Of the kinases in the panel, 14 kinases have an IC50 below 10 μM, but only 2 non-JAK kinases have IC50 values below 1 μM (Rock1 at 0.92 μM and Rock2 at 0.43 μM). JAK activity assays using isolated kinase domains in the presence of 0.1 mM ATP and trFRET kinome profiling were conducted as described previously (17). ATP, adenosine triphosphate; HTRF, homogenous trFRET; IC50, concentration producing 50% inhibition; JAK, Janus kinase; trFRET, time-resolved fluorescence energy transfer. (DOCX 22 kb)